1. PI3K/Akt/mTOR Apoptosis
  2. Akt Apoptosis
  3. AKT inhibitor VIII

AKT inhibitor VIII  (Synonyms: AKTi-1/2)

Cat. No.: HY-10355 Purity: 98.74%
COA Handling Instructions

AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

For research use only. We do not sell to patients.

AKT inhibitor VIII Chemical Structure

AKT inhibitor VIII Chemical Structure

CAS No. : 612847-09-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 161 In-stock
Solution
10 mM * 1 mL in DMSO USD 161 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 190 In-stock
50 mg USD 550 In-stock
100 mg USD 858 In-stock
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of AKT inhibitor VIII:

Top Publications Citing Use of Products

37 Publications Citing Use of MCE AKT inhibitor VIII

WB

    AKT inhibitor VIII purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Sep 23;10(10). pii: E1366.  [Abstract]

    Competition tests of SC79, PHT-427, AT7867, and AKT inhibitor VIII with the CGA probe against enriched AKT by CGA-modified functionalized MMs. Bands of AKT are detected by Western blot.

    AKT inhibitor VIII purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 May 25;8(5):e2817.  [Abstract]

    Injury-induced follicular activation is blocked by the mTOR inhibitor rapamycin. Mice are treated with specific inhibitors of the signaling pathways 12 h before surgery and another injection is given just after the surgery. Ovaries are collected at 6 h or 3 weeks after the surgery. C, control ovaries; S, surgically treated ovaries; Rapamycin, mTORC1 inhibitor; Akt VIII, Akt inhibitor; U0126, MAPK inhibitor. Specific inhibition of corresponding signaling pathways by inhibitors. Ovaries are collec

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

    IC50 & Target[1]

    Akt1

    58 nM (IC50)

    Akt2

    210 nM (IC50)

    Akt3

    2119 nM (IC50)

    In Vitro

    When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin[1]. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions[2]. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    551.64

    Formula

    C34H29N7O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1NC2=CC=CC=C2N1C3CCN(CC4=CC=C(C5=NC6=CC(NC=N7)=C7C=C6N=C5C8=CC=CC=C8)C=C4)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (36.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8128 mL 9.0639 mL 18.1278 mL
    5 mM 0.3626 mL 1.8128 mL 3.6256 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.97%

    References
    Cell Assay
    [3]

    PSC are plated onto Matrigel coated 96-well plates at densities between 1×103-3×105 cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8128 mL 9.0639 mL 18.1278 mL 45.3194 mL
    5 mM 0.3626 mL 1.8128 mL 3.6256 mL 9.0639 mL
    10 mM 0.1813 mL 0.9064 mL 1.8128 mL 4.5319 mL
    15 mM 0.1209 mL 0.6043 mL 1.2085 mL 3.0213 mL
    20 mM 0.0906 mL 0.4532 mL 0.9064 mL 2.2660 mL
    25 mM 0.0725 mL 0.3626 mL 0.7251 mL 1.8128 mL
    30 mM 0.0604 mL 0.3021 mL 0.6043 mL 1.5106 mL
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    AKT inhibitor VIII Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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